Histone Acetyltransferase Inhibitor

DS17701585 (Compound 11) is a highly selective, orally active EP300 and CBP inhibitor with IC₅₀ values of 0.040, 0.15, 0.45 and 0.70 µM against CBP, EP300, H3K27 and SOX2. DS17701585 can be used for cancer research.

CPI-644 is a selective EP300/CBP bromodomain inhibitor, with an IC₅₀ of 0.18 µM against the CBP bromodomain. CPI-644 reduces the proportion of FOXP3⁺ cells and downregulates the expression of LAG-3, CTLA-4 and PD-1. CPI-644 can be used in cancer-related research.

CBP/p300-IN-14 is a potent inhibitor of CBP/EP300 (lysine acetyltransferase) with an IC₅₀ of 3.3 nM (extracted from patent WO2021213521A1, compound 27).

CBP/p300-IN-18 (compound 8) is a potent EP300/CBP HAT inhibitor with IC₅₀s of 0.056, 0.46 µM for HAT EP300 and LK2 H3K27, respectively.

Ep300/CREBBP-IN-4 (Example 56) is a potent Ep300 and CREBBP inhibitor with IC₅₀s of 0.024 and 0.064 μM, respectively. Ep300/CREBBP-IN-4 can be used for the research of cancer.

CZL-149 is an orally active dual BET and p300/CBP bromodomains inhibitor with IC₅₀s of 13 nM and 10.5 nM for BED4 BD1 and p300, respectively. CZL-149 reduces c-Myc and H3K27Ac levels. CZL-149 has good drug-like properties and metabolic characteristics, as well as good safety. CZL-149 can be used for the study of multiple myeloma.

EP300/CBP-IN-2 is a potent EP300/CBP inhibitor that has good activity in vivo. EP300/CBP-IN-2 can be used for the research of cancer.

CBP/p300-IN-21 (Compound 5d) is a selective CBP/p300 inhibitor (IC₅₀: 0.07 and 1.755 μM for p300 and CBP). CBP/p300-IN-21 decreases H3K18Ac level. CBP/p300-IN-21 inhibits growth of 4T1 tumor growth in mice.

CBP/p300-IN-15 (compound 13a) is a potent p300/CBP inhibitor, with IC₅₀ values of 2.50 and 28.0 nM, respectively. CBP/p300-IN-15 shows good activity against OVCAR-3 and A2780 cell line, with EC₅₀ values of 0.865 and 2.71 μM, respectively. CBP/p300-IN-15 can be used for ovarian cancer research.

CTK7A is a curcumin derivative with anticancer activity by inhibiting the HAT activity of p300 and reducing the autoacetylation of p300, thereby affecting its interaction with HIF-1α. The inhibition of CTK7A leads to decreased HIF-1α accumulation and activity, which can be used for cancer research.

KAT6A/KAT7-IN-2 is a KAT6A and KAT7 inhibitor. KAT6A/KAT7-IN-2 has IC₅₀ values of both ≤ 1 nM for KAT6A and KAT7. KAT6A/KAT7-IN-2 can inhibit the acetylation of H3K14 and H3K23. KAT6A/KAT7-IN-2 also inhibits tumor cell proliferation. KAT6A/KAT7-IN-2 can be used in the study of cancer.

CBP-IN-1 is a potent CBP inhibitor with an IC₅₀ of 1.5 nM. CBP-IN-1 also inhibits CBP BRET and BRD4 (1), with IC₅₀ values of 690 nM and 3100 nM, respectively. CBP-IN-1 can be used in oncology and immuno-oncology research.

KB528 is a p300/CBP histone acetyltransferase (KAT) inhibitor with low nM IC₅₀ values against human p300 and CBP, and exhibits selectivity over other KAT family members. KB528 modulates the IRF4 transcriptional network, downregulates the expression of IRF4, MYC, CAV2 and IGLL5, and reduces the protein level of IKZF3. KB528 potently induces apoptosis in multiple myeloma cells. KB528 is applicable to research related to multiple myeloma.

Ep300/CREBBP-IN-3 (Example 61) is a potent Ep300 and CREBBP inhibitor with IC₅₀s of 0.056 and 0.095 μM, respectively. Ep300/CREBBP-IN-3 can be used for the research of cancer.

P300 bromodomain-IN-1 (Compoun 1u) is a potent p300 (EP300) bromodomain inhibitor with an IC₅₀ of 49 nM. P300 bromodomain-IN-1 suppresses the expression of c-Myc and induces G1/G0 phase arrest and apoptosis in OPM-2 cells.

KAT6A/KAT7-IN-1 is a KAT6A and KAT7 inhibitor with IC₅₀ for KAT6A of within the range of 1-10 nM, and for KAT7 of ≤ 1 nM. KAT6A/KAT7-IN-1 can inhibit the acetylation of H3K14 and H3K23. KAT6A/KAT7-IN-1 can be used in the research of breast adenocarcinoma.

CBP/p300-IN-16 (compound 1) is a potent EP300/CBP HAT inhibitor with IC₅₀s of 0.61, 2.24 µM for HAT EP300 and LK2 H3K27, respectively.

P300-IN-5 is a biological inhibitor that demonstrates potent activity against histone acetyltransferases (HAT) both in vitro and in vivo. P300-IN-5 may serve as an alternative therapeutic agent, especially in contexts requiring caution, such as during breastfeeding.

CBP/EP300 bromodomain receptor-IN-1 (Compound 10) is an inhibitor for CBP/EP300 bromodomain receptor, which binds to proteins having a bromodomain in nanomolar level.

BRD-IN-3 ((R,R)-36n) is a highly potent PCAF bromodomain (BRD) inhibitor, with an IC₅₀ of 7 nM. BRD-IN-3 also exhibits activity against GCN5 and FALZ.